Comparative disposition of tripelennamine in horses and camels after intravenous administration.

The pharmacokinetics of tripelennamine (T) was compared in horses (n = 6) and camels (n = 5) following intravenous (i.v.) administration of a dose of 0.5 mg/kg body weight. Furthermore, the metabolism and urinary detection time was studied in camels. The data obtained (median and range in brackets) in camels and horses, respectively, were as follows: the terminal elimination half-lives were 2.39 (1.91-6.54) and 2.08 (1.31-5.65) h, total body clearances were 0.97 (0.82-1.42) and 0.84 (0.64-1.17)L/h/kg. The volumes of distribution at steady state were 2.87 (1.59-6.67) and 1.69 (1.18-3.50) L/kg, the volumes of the central compartment of the two compartment pharmacokinetic model were 1.75 (0.68-2.27) and 1.06 (0.91-2.20) L/kg. There was no significant difference (Mann-Whitney) in any parameter between camels and horses. The extent of protein binding (mean +/- SEM) 73.6 + 8.5 and 83.4 +/- 3.6% for horses and camels, respectively, was not significantly statistically different (t-test). Three metabolites of T were identified in urine samples of camels. The first one resulted from N-depyridination of T, with a molecular ion of m/z 178, and was exclusively eliminated in conjugate form. This metabolite was not detected after 6 h of T administration. The second metabolite, resulted from pyridine ring hydroxylation, had a molecular ion of m/z 271, and was also exclusively eliminated in conjugate form. This metabolite could be detected in urine sample for up to 12 h after T administration. The third metabolite has a suspected molecular ion of m/z 285, was eliminated exclusively in conjugate form and could be detected for up to 24 h following T administration. T itself could be detected for up to 27 h after i.v. administration, with about 90% of eliminated T being in the conjugated form.

The pharmacokinetics of pentazocine and tripelennamine.

The pharmacokinetics of single and combined doses of pentazocine HCl (40 and 80 mg) and tripelennamine HCl (50 and 100 mg) were studied in six healthy drug abusers. After intramuscular administration of 40 or 80 mg pentazocine alone, mean peak plasma concentrations at 15 minutes were 102 and 227 ng/ml, respectively, and mean plasma t1/2 values were 4.6 and 5.3 hours, respectively. After intramuscular administration of 50 or 100 mg tripelennamine, mean plasma concentrations at 30 minutes were 105 and 194 ng/ml, respectively, and mean plasma t1/2 values were 2.9 and 4.4 hours, respectively. After concurrent administration of pentazocine with tripelennamine, plasma pentazocine and tripelennamine concentrations at all time points were not significantly different from those when pentazocine or tripelennamine was administered alone. Coadministration of pentazocine and tripelennamine had no effect on the distribution, elimination, and clearance of either pentazocine or tripelennamine. In conclusion, there did not appear to be a clinically significant metabolic interaction between pentazocine and tripelennamine.

Pentazocine and tripelennamine (T's and Blues) abuse: toxicological findings in 39 cases.

The post mortem findings of pentazocine and tripelennamine ("T's and Blues") in abusers dying in the City of St. Louis between July 1, 1979 and July 30, 1981 are presented. Thirty-three deaths were homicides; 30 black males, ages 21-38; one white male, age 26, died from gunshot wounds; and two black females, age 18 and 32, died of stab wounds. Blood concentrations of pentazocine and tripelennamine in these cases ranged from 0.20 to 3.3 mg/L, (mean +/- SD 0.72 +/- 0.64 mg/L) and 0.02 to 1.8 mg/L (mean +/- SD 0.29 +/- 0.40 mg/L), respectively. The six deaths attributed to T's and Blues abuse involved three black males, ages 20, 28 and 49, and three black females, ages 21, 25, and 45 years. Blood concentrations of pentazocine and tripelennamine ranged from 0.44 to 2.5 mg/L and 0.09 to 4.1 mg/L, respectively. Ethanol and diazepam were also detected in 49% and 13% of all deaths, respectively. Foreign body or talc granulomas in lung were the most common pathological finding relevant to the abuse of T's and Blues.

Determination of pentazocine and tripelennamine in blood of T's and Blue addicts by gas-liquid chromatography with a nitrogen detector.

A procedure for the quantitative determination of pentazocine (T's) and tripelennamine (Blues) in blood obtained from T's and Blues addicts is described. The underivatized drugs were analyzed by gas-liquid chromatography with a nitrogen detector. The retention times relative to mepivicaine (internal standard) on OV-17 at 220 degrees C were: tripelennamine 0.69 and pentazocine 1.77. The linear ranges of blood standards were: tripelennamine, 0.10-1.00 microgram/ml; pentazocine, 0.50-5.0 microgram/ml. For simultaneous analysis, the within-run and between-run CVs of tripelennamine were 5.6% (n = 23) and 13% (n = 12); and for pentazocine 5.2% (n = 23) and 9.9% (n = 12). Mean recoveries over the range of standards were: tripelennamine, 103% +/- 2.5% (n = 12); pentazocine 77.8% +/- 3.6% (n = 12).